| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C24H29N7O5 |
| Purity | |
| Activity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
WYE-354 is an ATP-competitive inhibitor of mTOR, acting with an IC50 of 5 nM. It also inhibits PI3Kα and PI3Kγ, with IC50 values of 1.89 μM and 7.37 μM, respectively, and blocks both mTORC1 and mTORC2. In vitro, WYE-354 induces autophagy activation[3]. It is supplied as a white to off-white solid (C24H29N7O5, MW 495.53) at 98.03% purity.
Physical & Chemical Properties
| CAS Number | 1062169-56-5 |
|---|---|
| Molecular Formula | C24H29N7O5 |
| Molecular Weight | 495.53 g/mol |
| Purity | 98.03% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | COC(NC1=CC=C(C=C1)C2=NC3=C(C(N4CCOCC4)=N2)C=NN3C5CCN(CC5)C(OC)=O)=O |
| Target | mTOR, mTORC1, mTORC2, PI3K alpha, PI3K gamma |
| Signaling Pathway | PI3K/Akt/mTOR; Autophagy; Apoptosis |
| Bioactivity Class | Autophagy |
| Solubility | In Vitro: DMSO: 6.67 mg/mL (13.46 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
mTOR 5 nM (IC50) |
PI3K alpha 1.89 μM (IC50) |
PI3K gamma 7.37 μM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 6.67 mg/mL (13.46 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 0.67 mg/mL (1.35 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 0.67 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (6.7 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 0.67 mg/mL (1.35 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 0.67 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (6.7 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 0.67 mg/mL (1.35 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 0.67 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (6.7 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
WYE-354 inhibits recombinant mTOR enzyme with an IC50 of 5 nM in the DELFIA that measures His6-S6K1 T389 phosphorylation[1]. Viability is assessed by MTS assay after G-415 and TGBC-2TKB cells are exposed for 24, 48, and 72 hours to rising concentrations of WYE-354 (0.1, 1, 5 and 10 μM). In both cell lines, WYE-354 significantly lowers cell viability from 1 μM onward after 24 hours of exposure (P<0.001). No decrease in viability appears at 100 nM, except in TGBC-2TKB cells after 72 hours of treatment[2].
In Vivo
Tumor growth effects of Rapamycin and WYE-354 are evaluated in xenograft GBC tumor models. G-415 or TGBC2TKB cells, 2×106 or 5×106 respectively, are xenotransplanted subcutaneously into NOD-SCID mice. Once tumors reach an average volume of 100 mm3, the mice receive either Rapamycin or WYE354. Rapamycin is given i.p. at 10 mg/kg daily, 5 days per week for 3 weeks, while WYE-354 is given i.p. at 50 mg/kg daily for 5 days. Mice are sacrificed 30 days after the start of treatment, followed by an autopsy that includes removal of the entire tumor area. WYE-354-treated mice show 68.6% and 52.4% reductions in average tumor size (P<0.01; P<0.01), and 82.9% and 45.5% reductions in tumor weight (P<0.01; ns), respectively[2].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Cell Assay[2]
Plate G-415 and TGBC-2TKB cells at 2×103 cells per well onto 96 well plates. After overnight attachment, treat the cells with WYE-354. Determine the number of viable cells at set intervals with the CellTiter 96 Aqueous One Solution Cell Proliferation assay: add 20 μL CellTiter 96 solution to each well, incubate the plates for 2 hour, then read the absorbance of each well at 490 nm using a multiwell plate reader. Perform all assays in quintuplicate and repeat each assay three times[2].
Animal Administration[2]
Mice[2] Inject 8 to 12-week-old NOD-SCID mice subcutaneously in one flank with G-415 or TGBC2TKB cells (2×106 or 5×106 cells, respectively) resuspended in 200 μL of PBS containing 30% Matrigel. Once the average tumor reaches 100 mm3, randomly separate the mice into four groups and treat with Rapamycin or WYE-354 and their respective vehicles. Give Rapamycin intraperitoneally (i.p) at 10 mg/kg daily, 5 days per week for 3 weeks, and WYE-354 at 50 mg/kg i.p daily for 5 days. Estimate tumor volumes twice a week.
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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GSFM: A genome-scale functional module transformation to represent drug efficacy for in silico drug discovery. Acta Pharm Sin B 2025 Jan;15(1):133-150. PMID: 40041913
Overexpression of ABCB1 Transporter Confers Resistance to mTOR Inhibitor WYE-354 in Cancer Cells. Int J Mol Sci 2020 Feb 19;21(4):1387.
CC-223, NSC781406, and BGT226 Exerts a Cytotoxic Effect Against Pancreatic Cancer Cells via mTOR Signaling. Front Pharmacol 2020 Nov 11:11:580407. PMID: 33343350
In Vitro and in Vivo Activity of mTOR Kinase and PI3K Inhibitors Against Leishmania donovani and Trypanosoma brucei. Molecules 2020 Apr 23;25(8):1980.
Low shear stress induces vascular eNOS uncoupling via autophagy-mediated eNOS phosphorylation. Biochim Biophys Acta Mol Cell Res 2018 May;1865(5):709-720.
Selective ATP-competitive inhibitors of TOR suppress rapamycin-insensitive function of TORC2 in Saccharomyces cerevisiae. ACS Chem Biol 2012 Jun 15;7(6):982-7.
bioRxiv. 2024 September 07.
